发明授权
- 专利标题: 3-Methylene cephalosporanic acid derivatives and process for preparation thereof
- 专利标题(中): 3-亚甲基头孢菌酸衍生物及其制备方法
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申请号: US841321申请日: 1977-10-11
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公开(公告)号: US4138553A公开(公告)日: 1979-02-06
- 发明人: Sachio Ishimoto , Hisao Yamaguchi , Yoshinori Kato , Takeo Oba , Kenji Ozawa , Yataro Ichikawa , Koji Nakagawa , Hideki Tsuruta
- 申请人: Sachio Ishimoto , Hisao Yamaguchi , Yoshinori Kato , Takeo Oba , Kenji Ozawa , Yataro Ichikawa , Koji Nakagawa , Hideki Tsuruta
- 申请人地址: JPX Osaka
- 专利权人: Teijin Limited
- 当前专利权人: Teijin Limited
- 当前专利权人地址: JPX Osaka
- 主分类号: C07D499/00
- IPC分类号: C07D499/00 ; C07D501/10 ; C07D501/02
摘要:
Novel substituted hydrazide derivatives of 7-(substituted)amino-3-methylene-cepham-4-carboxylic acids expressed by the formula ##STR1## wherein R.sub.1 represents alkyl containing at least 3 carbon atoms, cycloalkyl, or optionally substituted aryl, and one of R.sub.2 and R.sub.3 represents hydrogen with the other being hydrogen or the same as R.sub.1 ; or R.sub.1 and R.sub.2 form a heterocyclic ring optionally through a hetero atom together with the attached nitrogen and R.sub.3 represents hydrogen atom; and Z.sub.1 represents amino or protected amino; and acid addition salts thereof, which are useful as intermediates for synthesizing cephalosporin antibiotics. These compounds can be prepared in high yields from the corresponding substituted hydrazide derivatives of 6-substituted amino-1-oxide-2, 2-dimethyl-penam-3-carboxylic acids, which are readily available at low costs, by heating them in the presence of a thermal rearrangement promotor such as organic sulfonic acids and optionally in the further presence of a tertiary nitrogen-containing cyclic compound, followed if desired by splitting off the amino-protecting group and converting the product to acid addition salts.
公开/授权文献
- US4750104A Method of and apparatus for tracking position error control 公开/授权日:1988-06-07
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